Immediate release film coatings containing medium chain glycerides and substrates coated therewith

ABSTRACT

The present invention is directed to immediate release film coating compositions for use on oral dosage forms such as compressed tablets and other orally-ingestible substrates which contain medium chain glycerides as detackifiers. The film coating compositions can be applied either directly to a substrate or after the substrate has been coated with a subcoat. In preferred aspects, the polymer is polyvinyl alcohol and the medium chain glycerides are mixtures of caprylic (8 carbon chain) and capric (10 carbon chain) mono- and diesters of glycerin. Aqueous suspensions comprising the inventive film coating compositions, methods of applying the coatings to substrates and the coated substrates themselves are also disclosed.

CROSS-REFERENCE TO RELATED APPLICATIONS

This application claims the benefit of priority from U.S. ProvisionalApplication Ser. No. 61/929,735, filed Jan. 21, 2014, the contents ofwhich are incorporated herein by reference.

1. FIELD OF THE INVENTION

The present invention relates to immediate release film coatingformulations which contain medium chain glycerides as detackifiers. Theinvention also relates to pharmaceutical substrates having such filmcoatings and methods of preparing the same.

2. BACKGROUND OF THE INVENTION

The use of detackifiers in film coating compositions is described in theprior art for both immediate release and enteric film coatingapplications. Commonly assigned U.S. Pat. No. 8,388,983 describes filmcoating formulations, which comprise fine particle size detackifiersthat are practically insoluble in water. These detackifiers are in solidform at room temperature, alone, as part of a film coating formulation,and when dispersed in water. While film coatings containing these fineparticle size detackifiers have many advantages such as good moisturebarrier and high productivity, occasional aesthetic issues have beenobserved when using these coatings. The practically water-insoluble,fine particle size detackifiers may be present in logos on dosage formsor may be observed as specks on tablet surfaces, especially when thecolor of the coating is dark.

Accordingly, there is still a need for improved film coatingcompositions which have the advantages of good moisture barrierproperties and high productivity. The present invention addresses thisneed.

3. SUMMARY OF THE INVENTION

It has been surprisingly found that immediate release film coatingformulations comprising medium chain glycerides as detackifiers arewell-dispersed in ambient temperature water and, when coated ontopharmaceutical compositions, completely disintegrate in less than twohours in both simulated gastric and intestinal fluids. Use of theinventive film coatings on oral substrates such as tablets results inimproved product appearance, for example, in terms of reduced amounts ofvisible specks, as well as comparable or better moisture barrierperformance of formulated coating systems when compared to that of theprior art.

The present invention relates to the development of fully-formulatedfilm coating systems containing medium chain glycerides as detackifiers.The invention further relates to aqueous dispersions comprising themedium chain glycerides, methods of preparing the same by dispersing thefilm coating materials (system) in ambient temperature water and orallyingestible substrates having the inventive film coating comprising themedium chain glycerides dried thereon.

In one aspect of the invention, there are provided powder film coatingcompositions for the pharmaceutical and related arts. The preferably drypowder film coating compositions include one or more polymers, such aspolyvinyl alcohol (hereinafter sometimes abbreviated as “PVA”), mediumchain glycerides as detackifiers and optionally plasticizers, glidants,pigments and other additives commonly used in film coating formulations.In preferred aspects of this invention, the medium chain glyceridescomprise a mixture of caprylic (8 carbon chain) and capric (10 carbonchain) mono- and diesters of glycerin.

In another aspect of the invention, there are provided aqueousdispersions of the film coating compositions described above that areprepared in ambient temperature water. The dispersions preferablycontain from about 5 to about 40% non-water ingredients content. Stillfurther aspects include methods of coating orally-ingestible substrateswith the coating suspension as well as the coated substrates prepared bythese methods.

In the preferred aspects of this invention, immediate release filmcoatings are prepared that completely disintegrate within 2 hours inboth simulated gastric and intestinal fluids when coated ontoorally-ingestible substrates in the amounts (weight gains) describedherein. Furthermore, the coated ingestible substrates have low levels ofvisible specks on the surfaces of the coated orally-ingestiblesubstrates, particularly in debossed or intagliated regions which maycontain logos or the like. This combination of properties for animmediate release film coating system is clearly advantageous over theprior art and existing marketed products.

4. DETAILED DESCRIPTION OF THE INVENTION

For purposes of the present invention, the following terms are givenfurther clarification as to their meanings:

-   -   “orally-ingestible substrate” shall be understood to mean any        pharmaceutically acceptable dosage form, e.g. tablet, capsule,        caplet, etc. or any other veterinary or confectionary product        intended to be swallowed;    -   “dry powder” shall be understood to mean powders which are        relatively dry to the touch rather than powders which are        essentially without liquid content;    -   “ambient temperature” shall be understood to mean temperatures        generally in the range of from about 20° C. (68° F.) to about        30° C. (86° F.)+/−3° C.;    -   “glycerin” is synonymous with “glycerol”, and “glycerol esters”        is synonymous with glycerides;    -   “simulated gastric fluids” are media having a pH from about 1 to        about 5.5, which may be buffered or unbuffered, with or without        enzymes; and    -   “simulated intestinal fluids” are media having a pH from about        5.5 to about 8, which may be buffered or unbuffered, with or        without enzymes.

The inventive film coating compositions comprise one or more polymers,medium chain glycerides and optionally glidants, pigments, surfactantsor other film coating auxiliaries.

The polymer may be any of the commonly used immediate release filmformers in the film coating art. These may include hypromellose(hydroxypropyl methylcellulose), hydroxypropyl cellulose, sodiumcarboxymethyl cellulose, polyvinyl alcohol (PVA), and copolymers basedon PVA. A preferred grade of PVA is one prepared by hydrolyzing 86.5 to89 mol % of the acetate groups on polyvinyl acetate. PVA copolymers mayinclude PVA-polyethylene glycol graft copolymers such as those soldunder the KOLLICOAT IR trade name or PVA-methyl methacrylate-acrylicacid copolymers such as those sold under the POVACOAT trade name. Insome aspects, the polymers are of sufficiently small particle size,preferably less than 250 microns, to facilitate dissolution into ambientwater when forming the aqueous coating solutions. Two or more of thesepolymers may be used together. PVA is a preferred polymer for manyaspects of the invention.

In most embodiments, the amount of polymer included in the powdermixtures of the present invention is from about 20 to about 70% byweight. In some preferred embodiments, it ranges from about 25 to about60% and more preferably ranges from about 30 to about 50%. When two ormore polymers are used together, the combined total of the polymers isfrom about 20 to about 70% by weight. Also, when two or more polymersare used, the preferred total amount of polymers is from about 25 to 60%and more preferably from about 30 to about 50%.

The medium chain glycerides may be monoesters, diesters and triesters ofglycerin with saturated aliphatic carboxylic acids having from 6 to 10carbon atoms. Examples of such acids include straight chain acids suchas hexanoic acid, heptanoic acid, octanoic acid (also known as caprylicacid), nonanoic acid and decanoic acid (also known as capric acid) aswell as branched aliphatic carboxylic acids with a total carbon contentof 6 to 10 atoms. The most preferred monoesters, diesters and triestersof glycerin remain in the liquid state at ambient temperatures. When adiester or triester of glycerin is employed, the carboxylic acidmoieties on each molecule may be the same or different. Mixtures ofesters, which may be monoesters, diesters and or triesters withdifferent carboxylic acids, may also be employed.

In general, carboxylic acid esters of glycerin are mixtures of themonoester, diester and triester. Monoesters and diesters are preferreddue to the presence of hydroxyl groups as will be explained later.Often, when preparing esters of glycerin, the mono-, di- and triestersare formed together. The relative ratio of the esters will depend uponthe manufacturing conditions and the proportion of reagents. Triestersmay be removed from the mixture, but it is often not economicallypractical from a manufacturing standpoint to completely remove alltraces of the triester. Therefore, many commercial monoester and diesterproducts contain a low level of triesters- for example, up to 10% byweight, i.e. 90% by weight mono and diesters of glycerin.

Likewise, in many cases, there may be small amounts of unreactedglycerin (up to about 10%) in commercial monoester and diester products.The presence of glycerin at these low levels does not appreciably affectthe properties of the mono- and diesters. Medium chain glycerides mayalso contain small amounts (up to 10% by weight) of higher molecularweight esters of glycerin without adversely affecting their properties.These may include carboxylic acids having 11-18 carbon atoms. It ispreferred that the medium chain glycerides remain in the liquid state atambient temperatures.

In most preferred aspects of the invention, the medium chain glyceridescomprise a mixture of caprylic (8 carbon chain) and capric (10 carbonchain) mono- and diesters of glycerin. Glycerol monocaprylocaprates arepreferred. Glycerol monocaprylocaprate Type I as listed in the EuropeanPharmacopoeia (EP) is one such example and is available under the tradename, Imwitor 742, from Cremer Oleo, GmbH and Co. KG, Hamburg, Germany.Alternative suppliers include Abitec, of Columbus Ohio with productsavailable under the trade names Capmul MCM, EP and Capmul MCM, NF.Glycerol monocaprylocaprate Type I comprises 45-75% monoesters, 20-50%diesters, less than 10% triesters and less than 3% free glycerin. Thecarbon chain distribution is 50-90% C8 (or 8 carbons), 10-50% C10, lessthan 3% C12 and less than 1% C14. Another preferred glycerolmonocaprylocaprate comprises 49-61% monoesters and 7% or less of freeglycerin.

The medium chain glycerides are primarily used as detackifiers to reducethe incidence of tablet-to-tablet sticking that can occur during thefilm coating of pharmaceutical tablets and the like using aqueoussuspensions/dispersions based on the inventive compositions. While notwishing to be bound by any particular theory, it is believed that themono- and diesters function well as detackifiers for the polymers,because they possess both free hydroxyl groups and carboxylic acidesters. The hydroxyl groups on the medium chain glycerides can formhydrogen bonds with the hydroxyl groups on the polymer chains, while themore hydrophobic ester groups act as barriers to limit extensiveassociation between polymer chains. Both mechanisms work together toprevent intermolecular associations between polymer chains that wouldotherwise lead to tackiness. The total amount of the medium chainglyceride detackifier present in the dry powder mixture will depend uponneed, but can broadly range from about 1 to about 30% by weight.Preferably, the range is from about 2 to about 15% and more preferablyfrom about 3 to about 7% by weight.

A glidant is optionally used to help tablets flow over each other and sogenerate a smooth surface finish. Talc and kaolin are preferredglidants. Preferred grades of talc have 90% of constituent particlesless than 50 microns to eliminate the presence of visible specks on thesurface of coated, orally-ingestible substrates. More preferred gradesof talc have 90% of constituent particles less than 20 microns tofurther reduce the presence of visible specks and also to enhancedispersion properties. The amount of glidant, when present, will dependupon need, but can broadly range from about 1 to about 50% by weight.Preferably, the range is from about 4 to about 40%, and, morepreferably, from about 10 to about 35%.

Pigments are also optionally added and may be any food orpharmaceutically approved colors, opacifiers or dyes. For example, thepigments may be aluminum lakes, iron oxides, titanium dioxide, naturalcolors or pearlescent pigments (e.g. mica based pigments sold under theCandurin trade name). Examples of such pigments are listed in U.S. Pat.No. 4,543,570, which is incorporated herein by reference. When included,the pigments may be used in the powder mixtures in a range (by weight)from about greater than 0 to about 40% pigment, preferably, from about 4to about 32% and, more preferably, from about 7 to about 30%. It will beunderstood, however, that the amount of pigment employed in the powdermixtures of the invention is an amount which is sufficient or effectiveto impart the required appearance of the outer coating to the surface ofthe substrate to be coated.

Furthermore, the powder mixtures may also include supplemental orauxiliary ingredients typically found in film coatings. A non-limitinglist of such adjuvants includes surfactants, suspension aids,sweeteners, flavorants, plasticizers etc. and mixtures thereof.Preferred surfactants are sodium lauryl sulfate and polysorbate 80.Sodium lauryl sulfate is a more preferred surfactant. The surfactant maybe included in the range of about 0.1 to about 5% in the dry filmcoating composition, and, more preferably between about 1 to about 4%.The use and function of the surfactant is to enhance the film formationprocess as commonly taught and used in the prior art.

The powder mixtures are prepared using standard dry blending or mixingtechniques known to those of ordinary skill. For example, theingredients are individually weighed, added to a suitable apparatus andblended for a sufficient time until a substantially uniform mixture ofthe ingredients is obtained. The time required to achieve suchsubstantial uniformity will, of course, depend upon the batch size andapparatus used. Addition of liquids such as the medium chain glycerideswill occur such that no significant agglomeration or separation willoccur. This can be accomplished by gradually adding the liquid mediumchain glycerides to the dry ingredients while blending. A preblend mayalso be utilized, wherein the liquid medium chain glycerides are firstadded to a portion of the dry ingredients and then the remaining drymaterial is added. The preblend may be prepared in bulk and used asneeded to reduce the mixing time required for smaller batches. In allcases, when the liquid medium chain glycerides are added to the dryingredients, the components must be mixed for a time sufficient toensure homogeneity.

As mentioned above, batch sizes will vary upon need. A non-limiting listof suitable blending devices include diffusion blenders such as a crossflow, V-blender, or hub blenders, available from Patterson-Kelly, orconvection blenders, such as Ruberg/Azo, Readco/CVM or Servoliftblenders may be used. Blending of the aforementioned formulations mayalso be achieved by processing ingredients into a granular form toproduce a non-dusting granular coating composition by methods including,but not limited to, wet massing, fluid bed granulation, spraygranulation and dry compaction, roller compaction or slugging. Othermanners of blending will be apparent to those of ordinary skill.

Some preferred dry film coating compositions in accordance with theinvention include:

Ingredient % by weight Preferred More Preferred Polymer (or polymers)20-70 25-60 30-50 e.g. PVA Medium chain glycerides  1-30  2-15  3-7 e.g. Glycerol mono- caprylocaprate Type I Glidant  0-50  4-40 10-35 e.g.talc, etc. Surfactant  0-5   1-4  — e.g. Na lauryl sulfate, etc.Pigments  0-40  4-32  7-30 Optional or aux.  0-20 — — ingredients

It will be understood from the foregoing table that the preferred dryfilm coating compositions will include at least a polymer and a mediumchain glyceride as described herein. The additional ingredients, ifincluded, will cause the amount of polymer and medium chain glyceride tobe reduced proportionally but both components will still be within theranges described herein, so that the total amount of all ingredients inthe dry blend will be 100% by weight.

For purposes of illustration and not limitation, an aqueous dispersionhaving about 20% non-water ingredients can be formed by dispersing 100grams of a blended powder mixture described hereinabove into 400 gramsof ambient temperature water. The water is weighed into a suitablevessel, i.e. one with a diameter approximately equal to the depth of thefinal suspension. A low shear mixer, preferably one having a mixingblade with a diameter about one third the diameter of the mixing vessel,is lowered into the water and turned on to create a vortex from the edgeof the vessel down to about just above the mixing blade to prevententrapment of air. The 100 grams of dry film coating composition isadded to the vortex at a rate where there is no excessive buildup of drypowder. The speed and depth of the mixing blade is adjusted to avoid airbeing drawn into the suspension so as to avoid foaming. The suspensionis stirred at low speed, preferably 350 rpm or less, for a timesufficient to ensure that a homogenous mixture is formed. Using theabove batch size as a guide, about 45 minutes mixing time is required.The suspension is then ready for spraying onto pharmaceutical substratesand the like. Those of ordinary skill will also realize that there aremany ways of preparing a substantially homogenous mixture of the solidsin water and that the scope of the invention is in no way dependent onthe apparatus used. It is contemplated that suitable aqueous dispersionswill contain from about 5 to about 40% and preferably from about 15 toabout 35% non-water ingredients therein.

In still further embodiments of the invention, there are providedorally-ingestible substrates coated with the inventive film coatingformulations. The coated substrates have excellent appearance anduniformity as well as enhanced stability in the presence ofenvironmental moisture and oxygen.

As will be described in the examples below, the methods include applyingthe film coating compositions as aqueous suspensions to the surfaces oforally ingestible substrates. The film coating can be applied as part ofa pan coating or spray coating process commonly used to coat sucharticles. The amount of coating applied will depend upon severalfactors, including the nature and functionality of the film coating, thesubstrate to be coated and the apparatus employed to apply the coating,etc. In some immediate release applications of the invention, thesubstrates will be tablets and will be coated to a theoretical weightgain of from about 0.25 to about 5.0%. Preferably, the theoreticalweight gain is from about 1.0 to about 4.5% and more preferably, thetheoretical weight gain is from about 2.0 to about 4.0% by weight ofsaid substrate. As mentioned above, the coating solutions of the presentinvention may also include auxiliary ingredients in addition to thepowder mixture and the water.

The coated, orally-ingestible substrates described above can alsoinclude a subcoat film coating between the orally-ingestible substrateand the inventive film coating comprising medium chain glycerides. Thesubcoat selected is preferably based on an edible film coatingcomposition that is compatible with and adheres to both theorally-ingestible substrate and the inventive coating. Thus, the artisanmay choose from a wide variety of pharmaceutical or food-acceptablecoatings for use as subcoats in the present invention. The subcoat isalso applied to the substrate to provide from about a 0.25 to about a5.0% weight gain to the orally-ingestible substrate.

Regardless of the method employed or the specific materials included inthe film coating compositions, the orally-ingestible substrates of thepresent invention will include a polymer and medium chain glycerides.

5. EXAMPLES

The following examples serve to provide further appreciation of theinvention but are not meant in any way to restrict the effective scopeof the invention. All ingredients are expressed as being by weight %.

Example 1

A preferred formulation for an inventive dry coating composition is thefollowing:

Component Parts by Weight PVA 37.0 Talc 31.0 Glycerol monocaprylocaprate4.0 Sodium lauryl sulfate 3.0 Titanium dioxide 20.0 Blue#2 aluminum lakepigment 5.0 100.0Preparation of the Dry Film Coating Composition:

The dry film coating composition was prepared by adding all dryingredients (PVA, talc, sodium lauryl sulfate and titanium dioxide) intoa laboratory blender and blending for 5 minutes until a homogenousmixture was produced. Glycerol monocaprylocaprate, the only liquidcomponent, was then gradually added to the dry mixture, and the totalmixture was blended for an additional 2 minutes after all liquid wasintroduced.

Preparation of the Aqueous Dispersion:

The dry film coating composition (100 grams) was dispersed into 400grams of ambient temperature water to make an aqueous coating suspensionhaving 20% w/w non-water ingredients. The water was weighed into avessel with a diameter approximately equal to the depth of the finaldispersion. A low shear mixer was lowered into the water and turned onto create a vortex from the edge of the vessel down to just above themixing blade to prevent entrapment of air. The 100 grams of dry filmcoating composition was added to the vortex at a rate where there was noexcessive buildup of dry powder or foam. The speed and depth of themixing blade was adjusted to avoid air being drawn into the suspensionso as to avoid foaming. The suspension was stirred at low speed (350 rpmor less) for 45 minutes to form a homogeneous aqueous dispersionsuitable for coating.

Coating of Tablets:

A 2.5 kilogram batch of convex placebo tablets (10 mm diameter) wasspray coated with the aqueous dispersion described above in an O'HaraLabCoat fully perforated side-vented coating pan equipped with a paninsert having a diameter of 15″ and one spray gun fitted with a nozzlehaving an aperture of 1 mm. The average coating parameters were: inlettemperature (IT) 76° C., exhaust temperature (ET) 48° C., coating bedtemperature (BT) 45° C., airflow 297 cubic meters/hr., differentialpressure −0.1 in. of water, atomizing air pressure (AP) 1.4 bar, panspeed (PS) 18 rpm. No tablet-to-tablet or tablet-to-coating pan stickingwas observed at a spray rate of 30 grams/minute. A theoretical coatingweight gain of 4.0% was applied to the tablets. The resulting coatedtablets were smooth, non-tacky and glossy.

Determination of Moisture Vapor Transmission Rate:

Moisture vapor transmission rate (MVTR) was determined by firstpreparing a cast film sample from the aqueous dispersion described aboveby sequentially spraying the dispersion onto a flat polyethyleneterephthalate (PET) surface secured on a metal plate heated to 60° C. A100 micron thick film was thus obtained for testing. MVTR of the filmwas measured on a Mocon PermaTran-W 1/50 unit where the sample wastested at an 80% RH gradient at 25° C. The MVTR for the cast filmprepared from the formulation of Example 1 was 95 grams H₂O/day/m².

Visual Assessment of Coated Tablets:

100 randomly selected tablets were carefully observed for the presenceof small white specks. Only 9 out of 100 tablets had at least one verysmall speck on the tablet surface. No logo filling was observed.

Disintegration Test:

Disintegration testing was performed in accordance with the USPDisintegration Method. Six tablets were prepared as described previouslyand placed in a basket assembly and immersed in either simulated gastricfluid (0.1N HCl, pH 1.2), or simulated intestinal fluid (pH 6.8phosphate buffer). The basket was moved up and down at a rate of about28-32 cycles/minute. The integrity of the tablets was evaluatedthroughout the testing period, and the time for the first and lasttablet to disintegrate noted. These values were then used to determinethe average disintegration time for the samples in each media. Theaverage disintegration time of the tablets in 0.1N HCl and pH 6.8phosphate buffer was 86 and 93 seconds, respectively.

Comparative Example A

A formulation similar to that in Example 1 was prepared except that theglycerol monocaprylocaprate was eliminated from the formulation, and thetalc level was increased to compensate.

Component Parts by Weight PVA 37.0 Talc 35.0 Glycerol monocaprylocaprate0.0 Sodium lauryl sulfate 3.0 Titanium dioxide 20.0 Blue#2 aluminum lakepigment 5.0 100.0

The aqueous dispersion preparation and coating process were conducted inan analogous fashion as that described in Example 1. The formulation didnot disperse well in the aqueous medium, and significant foaming wasobserved. 20-25 tablets were observed to be stuck to the inside of thecoating pan per revolution as the coating was being applied at a sprayrate of 30 grams/minute. 100 out of 100 tablets showed the presence ofvisible specks on the tablet surface, and logo filling was observed

Examples 2-12

Film coating compositions (100 grams each) and aqueous dispersionscomprising them were prepared by methods similar to those described inExample 1. Coating performance and tablet properties were similarlyassessed.

Example 2 3 4 5 6 Component % % % % % PVA 37.0 37.0 30.0 33.0 41.0 Talc33.0 29.0 38.0 35.0 27.0 Glycerol monocaprylocaprate 2.0 6.0 4.0 4.0 4.0Sodium lauryl sulfate 3.0 3.0 3.0 3.0 3.0 Titanium dioxide 20.0 20.020.0 20.0 20.0 Blue#2 aluminium lake pigment 5.0 5.0 5.0 5.0 5.0 Totals100 100 100 100 100 Performance Number of tablets stuck to coating 3-4 00 0 1 pan per revolution at a spray rate of 30 grams/minute Moisturevapor transmission rate 94 141 78 83 108 of films (grams H₂O/day/m²)Number of tablets showing white 67 11 26 21 14 specks (out of 100)Disintegration time (seconds) of coated tablets Simulated gastric fluid92 96 70 73 83 Simulated intestinal fluid 87 83 92 94 78

Examples 2-6 all showed that both the number of tablets showing whitespecks and the number of tablets sticking to the inside of the coatingpan decreased significantly versus Comparative Example A. The greatestimprovements were observed when the amount of glycerolmonocaprylocaprate was at least 4% of the composition.

Example 7 8 9* 10 Component % % % % PVA 37.0 37.0 26.0 Hypromellose (6cP viscosity) 37.0 Hypromellose (15 cP viscosity) 11.0 Talc 34.0 28.031.0 31.0 Glycerol monocaprylocaprate 4.0 4.0 4.0 4.0 Sodium laurylsulfate 0.0 6.0 3.0 3.0 Titanium dioxide 20.0 20.0 20.0 20.0 Blue#2aluminium lake pigment 5.0 5.0 5.0 5.0 Totals 100 100 100 100Performance Number of tablets stuck to coating pan per 1-2 1 0 1-2revolution at a spray rate of 30 grams/minute Moisture vaportransmission rate of films 82 75 171 71 (grams H₂O/day/m²) Number oftablets showing white specks 35 10 21 10 (out of 100) Disintegrationtime (seconds) of coated tablets Simulated gastric fluid 88 89 88 76Simulated intestinal fluid 94 91 79 97 *Due to viscosity limitations,the aqueous dispersion made from Example 9 contained 15 rather than 20%non-water components.

Examples 7-10 all showed that both the number of tablets showing whitespecks and the number of tablets sticking to the inside of the coatingpan decreased significantly versus Comparative Example A. This held truewhen the surfactant (sodium lauryl sulfate) level was varied and thepolymer type was changed.

A Example restated 11 12 Component % % % PVA 37.0 37.0 37.0 Talc 35.032.5 30.0 Glycerol monocaprylocaprate 4.0 4.0 Sodium lauryl sulfate 3.0Polysorbate 80 1.5 4.0 Titanium dioxide 20.0 20.0 20.0 Blue#2 aluminiumlake pigment 5.0 5.0 5.0 Totals 100 100 100 Performance Number oftablets stuck to coating pan per 20-25 1-2 4-5 revolution at a sprayrate of 30 grams/minute Moisture vapor transmission rate of films 92 86153 (grams H₂O/day/m²) Number of tablets showing white specks 100 16 8(out of 100) Disintegration time (seconds) of coated tablets Simulatedgastric fluid 95 88 87 Simulated intestinal fluid 105 102 94

Examples 11 and 12 showed that both the number of tablets showing whitespecks and the number of tablets sticking to the inside of the coatingpan decreased significantly versus Comparative Example A when thesurfactant type was changed.

Example 13 14 15 Component % % % Kollicoat IR (PVA-PEG graft copolymer)37.0 68.0 64.0 Talc 31.0 0.0 4.0 Glycerol monocaprylocaprate 4.0 4.0 4.0Sodium lauryl sulfate 3.0 3.0 3.0 Titanium dioxide 20.0 20.0 20.0 Blue#2aluminium lake pigment 5.0 5.0 5.0 Totals 100 100 100 Performance Numberof tablets stuck to coating pan per 0 1 1 revolution at a spray rate of30 grams/minute Moisture vapor transmission rate of films 126 397 326(grams H₂O/day/m²) Number of tablets showing white specks 35 0 0 (out of100) Disintegration time (seconds) of coated tablets Simulated gastricfluid 261 324 333 Simulated intestinal fluid 314 332 341

Examples 13-15 showed that both the number of tablets showing whitespecks and the number of tablets sticking to the inside of the coatingpan decreased significantly versus Comparative Example A when thepolymer was changed from PVA to Kollicoat IR and glycerolmonocaprylocaprate was used as the detackifier.

While there have been described what are presently believed to be thepreferred embodiments of the invention, those skilled in the art willrealize that changes and modifications may be made thereto withoutdeparting from the spirit of the invention. It is intended to claim allsuch changes and modifications that fall within the true scope of theinvention.

What is claimed is:
 1. An immediate release film coating composition inpowder form consisting essentially of a) a polymer selected from thegroup consisting of hypromellose (hydroxypropyl methylcellulose),hydroxypropyl cellulose, sodium carboxymethyl cellulose, polyvinylalcohol, copolymers based on polyvinyl alcohol, and mixtures thereof b)a detackifier selected from the group consisting of medium chainglycerides containing less than or equal to about 10% by weight oftriesters of glycerin, and c) a member of the group consisting ofglidants, pigments, surfactants and mixtures thereof.
 2. The immediaterelease film coating composition of claim 1, wherein the polymer ispolyvinyl alcohol, copolymers based on polyvinyl alcohol or a mixture ofpolyvinyl alcohol and copolymers based on polyvinyl alcohol.
 3. Theimmediate release film coating composition of claim 1, wherein themedium chain glycerides comprise a mixture of caprylic (8 carbon chain)and capric (10 carbon chain) mono- and diesters of glycerin.
 4. Theimmediate release film coating composition of claim 3, wherein themedium chain glycerides comprise glycerol monocaprylocaprate or glycerolmonocaprylocaprate Type I.
 5. The immediate release film coatingcomposition of claim 1, wherein the surfactant is sodium lauryl sulfate.6. The immediate release film coating composition of claim 1, whereinthe glidant is talc or kaolin.
 7. The immediate release film coatingcomposition of claim 1, wherein the polymer comprises 20-70% by weightof the composition.
 8. The immediate release film coating composition ofclaim 1, wherein a) the polymer is polyvinyl alcohol, b) the mediumchain glycerides comprise glycerol monocaprylocaprate, c) the glidant istalc, and d) the surfactant is sodium lauryl sulfate.
 9. The immediaterelease film coating composition of claim 1, wherein the medium chainglycerides comprise from about 1 to about 30% by weight of thecomposition.
 10. The immediate release film coating composition of claim9, wherein the medium chain glycerides comprise from about 2 to about15% by weight of the composition.
 11. The immediate release film coatingcomposition of claim 10, wherein the medium chain glycerides comprisefrom about 3 to about 7% by weight of composition.
 12. An aqueoussuspension comprising the immediate release film coating composition ofclaim 1 and water.
 13. An orally-ingestible substrate coated with theaqueous suspension of claim
 12. 14. The coated orally ingestiblesubstrate of claim 13, wherein the immediate release film coatingcomposition disintegrates or dissolves in less than two hours in mediawith a pH of 1 to
 8. 15. An immediate release film coating compositionin powder form consisting essentially of: a) a polymer selected from thegroup consisting of hypromellose (hydroxypropyl methylcellulose),hydroxypropyl cellulose, sodium carboxymethyl cellulose, polyvinylalcohol, copolymers based on polyvinyl alcohol and mixtures thereof; b)medium chain glycerides, wherein the medium chain glycerides compriseless than or equal to about 10% of triesters of glycerin; and c) amember of the group consisting of glidants, pigments, surfactants andmixtures thereof; wherein the polymer is present in the amount of 20-70%by weight; and the medium chain glycerides are present in the amount of1-30% by weight.
 16. The immediate release film coating composition ofclaim 15, wherein: a) the polymer is present in the amount of 25-60% byweight; b) the medium chain glycerides are present in the amount of2-15% by weight; c) the glidant is present in the amount of 4-40% byweight; d) the surfactant is present in the amount of 1-4% by weight;and e) the pigments are present in the amount of 4-32% by weight. 17.The immediately release film coating composition of claim 16, wherein:a) the polymer is present in the amount of 30-50% by weight; b) themedium chain glycerides are present in the amount of 3-7% by weight; c)the glidant is present in the amount of 10-35% by weight; and d) thepigments are present in the amount of 7-30% by weight.
 18. The immediaterelease film coating composition of claim 15, wherein the polymer ispolyvinyl alcohol.
 19. The immediate release film coating composition ofclaim 15, wherein the polymer is polyvinyl alcohol, copolymers based onpolyvinyl alcohol or a mixture of polyvinyl alcohol and copolymers basedon polyvinyl alcohol.